Other Sodium Channel Modulators

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SML0345 A 887826 ≥98% (HPLC) A-887826 is Nav1.8 channel blocker (IC50 = 11 nM) that blocks TTX-resistant sodium currents in rat dorsal root ganglion in a voltage dependent fashion. Oral administration of A-887826 to rats significantly attenuated tactile allodynia in a neuropathic pain model.
A3109 A-803467 ≥98% (HPLC) A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.
A9797 Ambroxol hydrochloride analytical standard Metabolite of bromhexine.
A Nav1.8-preferring sodium channel blocker
SML1093 Articaine hydrochloride ≥98% (HPLC) Articaine hydrochloride helps to alleviate pain and blocks transmission of the pain signal.
Articaine is an amide local anesthetic widely used in dentistry. Articaine acts by inhibition of nerve impulse conduction by blockade of sodium channels.
A2861 Astemizole ≥98% (HPLC) Astermizole is a potent hERG potassium channel blocker (IC50 of 0.9 nM) and may used as a pharmacological chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. It has also been studied for treatment of malaria, hERG and hEAG channel function in cancer and as a second generation antihistamine H-1 antagonist.
B2417 Benzamil hydrochloride hydrate ≥98% (HPLC) Selective and potent blocker of Na+/H+ and Na+/Ca2+ channels
E1501 Benzocaine ≥99% (HPLC)  
B5435 BIA 2-093 ≥98% (HPLC), solid Blocker of voltage-gated sodium channels; significantly blocks excitatory amino acid (glutamate and aspartate) release.
B5274 Bupivacaine hydrochloride monohydrate analytical standard, for drug analysis Sodium channel blocker, local anesthetic.
SML0057 Camostat mesylate ≥98% (HPLC) Camostat is a synthetic, orally bioavailble serine protease inhibitor.
Camostat mesylate (CM) is used to treat pancreatitis and reflux esophagitis after gastrectomy.
Camostat mesylate inhibits the production of TNF-α and monocyte chemoattractant protein-1 (MCP-1) by monocytes. It also inhibits the activity of pancreatic stellate cells. Camostat mesylate regulates the cytokine expression and inflammation and is effective in the treatment of dibutyltin dichloride-induced rat pancreatic fibrosis.
C4024 Carbamazepine powder Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
Carbamazepine is considered as a safe antiepileptic drug. It decreases the multiple drug therapy and maintains a better control of epilepsy.
C8981 Carbamazepine meets USP testing specifications Anticonvulsant; ligand for the GABAA receptor benzodiazepine modulatory site. Sodium channel inhibitor.
SML1360 Cariporide ≥98% (HPLC) Cariporide is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. Cariporide has shown cardioprotective and antiarrhythmic effects, and has recently been investigated for anticancer activity.
Cariporide, a sodium-hydrogen exchange inhibitor can decrease the liberation of myoglobin at the time of ischemia/reperfusion and reduces the liberation of NE (norepinephrine) during ischemia.
D8190 3′,4′-Dichlorobenzamil hydrochloride >98% (HPLC) Inhibits Na+/Ca2+ exchanger, Na+ transport and sarcoplasmic reticulum Ca2+ release channels.
D6035 Disopyramide phosphate salt Class IA antiarrhythmic; sodium channel blocker
SML1828 EMD-87580 ≥98% (HPLC) EMD-87580 is a selective inhibitor of the Na+/H+ exchanger subtype 1 (NHE-1), also known as the Na+/H+ antiporter. EMD-87580 has shown cardioprotective effects, and has been investigated as a possible treatment for Duchenne′s muscular dystrophy.
E9156 Encainide hydrochloride ≥98% (HPLC), powder Encainide hydrochloride is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative.
F6777 Flecainide acetate salt Class IC antiarrhythmic agent; sodium channel blocker
SML0874 GMQ hydrochloride ≥95% (HPLC) GMQ/2-Guanidine-4-methylquinazoline is a potent and selective modulator of acid-sensing ion channel (ASIC) that activates ASIC3 channels under neutral pH. GQM blocks acid-induced maximal peak current and alters ASICs pH dependence for activation and inactivation.
H9414 Halofantrine hydrochloride ≥98% (HPLC), solid Halofantrine is a blocker of delayed rectifier potassium current via the inhibition of hERG channel.
SML1035 ICA-121431 ≥98% (HPLC) ICA-121431 [2,2-diphenyl-N-(4-(N-thiazol-2-ylsulfamoyl)phenyl) acetamide, a small molecule inhibitor, targets the extracellular amino acids in S2 and S3 in VSDIV (domain IV voltage sensor), which is essential for Hm1a efficacy. In humans, ICA-121431 blocks TTX-sensitive Nav1.3 sodium channels upregulated in HEK-293 cells.
ICA-121431 is a potent, selective inhibitor of the human Nav1.3 and Nav1.1 voltage gated sodium channels (IC50 = 19 nM) with little or no activity against human Nav1.5 or Nav1.7 channels.
K4389 KR-32568 ≥98% (HPLC), solid Sodium/hydrogen exchanger-1 (NHE-1) inhibitor; IC50 = 0.23 μM; inhibited NHE-1-mediated rabbit platelet swelling; in anesthetized rats, reduced infarct size from 67% (control) to 43% (at 0.1 mg/kg) and 24% (at 1.0 mg/kg); reduced number of ventricular premature beats from 530 to 266 (at 0.1 mg/kg) and 115 (at 1.0 mg/kg); reduced ventricular fibrillation incidence from 17 to 8 (0.1 mg/kg) and 0 (1.0 mg/kg); implications for research and treatment of myocardial ischemic diseases.
L8288 Lappaconitine hydrobromide ≥96%, solid Selective blocker of the TTX-sensitive Na+ channels, without influence on the activation threshold of Na+ channels.
SML1092 Levobupivacaine hydrochloride ≥98% (HPLC) Levobupivacaine hydrochloride is a sodium channel blocker used as a long-acting local anaesthetic for epidural anesthesia. Levobupivacaine is the (S)-isomer of bupivacaine, with efficacy similar to that of bupivacaine with a reduced risk of cardiotoxicity.
L7757 Lidocaine powder Lidocaine, a neuroprotective agent, mediates blockage of sodium (Na+) channels. It prevents the influx of sodium ions leading to depolarization of sodium channels and metabolically inactivated in liver. Lidocaine has positive effect on cerebral ischemia. It is also used in the treatment of ventricular tachycardia. Lidocaine is an efficient anesthetic agent in ophthalmic surgeries as it is highly potent and has good tissue penetrability.
Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.
L1026 Lidocaine analytical standard Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration.
L5647 Lidocaine hydrochloride monohydrate solid Na+ channel blocker; class IB antiarrhythmic that is rapidly absorbed after parenteral administration
L1663 Lidocaine N-ethyl chloride Lidocaine N-ethyl chloride is an intracellular voltage-gated sodium channel blocker.
SML1025 Lorcainide hydrochloride ≥98% (HPLC) Lorcainide is a Class 1c antiarrhythmic agent that blocks open fast acting voltage-gated sodium channels (subtype Nav1.5). Data shows that Lorcainide is a potent, selective antagonists/inverse agonists of human and rat H3 histamine receptors.
SML0087 MEGX ≥95% (HPLC) MEGX is generated by hepatic cytochrome P-450 system upon oxidative de-ethylation. Measurement of MEGX by immunoassay contributes to liver function test. MEGX possesses antiarrhythmic action and therefore extends lidocaine effect.
Monoethylglycinexylidide (MEGX) is an active metabolite of lidocaine.
M1195 Metolazone ≥98% (HPLC), solid Inhibitor of thiazide-sensitive Na+-Cl- cotransporter; antihypertensive; moderate "loop" diuretic.
M2727 Mexiletine hydrochloride powder Class IB antiarrhythmic; sodium channel blocker
O3125 Ouabain octahydrate ≥95% (HPLC), powder Cardiac glycoside, inhibits Na(+)/K(+) ATPase, regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1. Ouabain resistance is associated with appearance of Na(+)/K(+) ATPase isoforms with low binding affinity.
Ouabain has its specific binding site on integral proteins of the plasma membrane. Heart disease is treated using ouabain derivatives. Increased ouabain production is observed during exercise in humans. Abnormally high levels of ouabain are indicated in congestive heart failure and hypertension. Ouabain signalling affects intracellular calcium levels, which is known to activate nuclear factor κB (NFκB).
PZ0274 PF-01247324 ≥98% (HPLC) In humans, PF-01247324 [6-amino-5-(2, 3, 5-trichloro-phenyl)-pyridine-2-carboxylic acid methylamide] prevents native tetrodotoxin-resistant (TTX-R) currents in dorsal root ganglion (DRG) neurons.
PF-01247324 is an orally bioavailable, selective and potent NaV1.8 channel blocker that inhibits that exhibits analgesic efficacy in rodent behavioral models of pain.
PZ0273 PF-04531083 ≥98% (HPLC) PF-04531083 is an orally available, potent and selective sodium channel Nav1.8 blocker. PF-04531083 was designated as a potential treatment of pain.
SML1061 PF-04856264 ≥98% (HPLC) PF-04856264 is a potent, selective inhibitor of the human Nav1.7 voltage gated sodium channel (IC50 = 28 nM). PF-04856264 blocks mouse Nav1.7 (IC50 = 131 nM) but has low potency against the rat Nav1.7 channel (IC50 = 4.2 mM).
PZ0210 PF-04885614 ≥98% (HPLC) PF-04885614 is a potent and selective Nav1.8 inhibitor.
PZ0311 PF-05089771 ≥98% (HPLC) PF-05089771 is a selective and potent inhibitor of the human voltage-gated sodium ion channel Nav1.7 with an IC50 value of 11 nM. PF-05089771 targets the voltage-sensing domain, preferentially interacting with, and stabilizing, inactivated channel conformations by interaction with the voltage-sensor domain (VSD) of Domain 4. Nav1.7 is expressed in sensory neurons and is critical for pain processing. PF-05089771 is being investigated for the treatment of chronic neuropathic pain.
PZ0297 PF-06305591 dihydrate ≥98% (HPLC) PF-06305591 is a potent and highly selective sodium channel Nav1.8 inhibitor.
P0026 Pilsicainide hydrochloride ≥98% (HPLC) Pilsicainide hydrochloride is a pure sodium channel blocker and an open channel blocker of Na+1 channels. Pilsicainide was defined as a pure sodium channel blocker. The compound is classified as a class Ic antiarrhythmic drug, and was originally developed in Japan. Similar to Lidocaine, Pilsicainide binds to open channels, but slowly. Pilsicainide is capable of selectively blocking the late currents in the mutant Na(+) channels that show dominant abnormal burst openings such as in δKPQ mutants. The compound is used to induce Brugada syndrome (BS) in animal models.
P6237 α-Pompilidotoxin >98% Voltage-gated sodium channel activator
P9879 Procaine hydrochloride ≥97% Procaine is a Na+ channel blocker, commonly used as an anesthetic agent and is considered safer than cocaine. It is also useful as a painkiller to treat pain, associated with joints and tendons.
P4670 Propafenone hydrochloride Blocks hKv1.5 and ATP-sensitive K+ channels; class 1C antiarrhythmic agent that is also an antagonist at β adrenergic receptors.
P0033 ProTx-II ≥95% (HPLC) ProTx-II is a potent, selective Nav1.7 blocker. Voltage-gated sodium channels (Nav) are responsible for transducing extracellular signals into action potentials in excitable cells. The Nav1 family consists of nine sub-types for which selective tools are highly valued. Discovery of subtype-selective tools has been challenging due to conservation of putative binding sites. Nav1.7 is expressed in sensory neurons and is critical for pain processing. ProTx-II, isolated from the tarantula Thrixopelma pruriens, is a potent blocker of Nav1 channels. Although ProTx-II blocks several members of this channel family, it has >100-fold selectivity for Nav1.7. ProTx-II is active in an in vitro model of pain processing. ProTx-II binds to a previously unknown site on the channel, conferring selectivity and increasing its value as a research tool. It blocks Nav1.7 by decreasing conductance and shifting the activation potential in the positive direction, resulting in an overall decrease in excitability.
82670 Pyrethrum extract ≥50% (sum of pyrethrines)  
Q3625 Quinidine anhydrous Class IA antiarrhythmic; potassium channel blocker.
Quinidine, an isomer of quinine has potential side effects like proarrhythmia on usage. It prolongs cardiac potential and is sodium channel blocker. It is a potential antagonist for α1-adrenoceptors and contributes to hypotension. It inhibits cytochrome P450 2D6 and improves circulation and brain penetration of dementia drug, dextromethorphan. Quinidine-dextromethorphan combination may be useful in treating pseudobulbar affect (PBA).
Q0875 Quinidine sulfate salt dihydrate Class IA antiarrhythmic; potassium channel blocker.
SML0378 Ralfinamide mesylate ≥98% (HPLC) Ralfinamide is a mixed sodium and N-type calcium channel blocker. Inhibiton is voltage-dependent, with higher potency against inactivated channels. Ralfinamide is two fold selective for tetrodotoxin (TTX)-resistant sodium channels compared with TTX-sensitive currents.
SML1139 Rostafuroxin ≥98% (HPLC) Rostafuroxin is a digitoxygenin derivative that selectively antagonizes the effects of endogenous ouabain on the Na+,K+-ATPase, which maintains sodium and potassium ion gradients across plasma membranes. Rostafuroxin lowers blood pressure (BP) in animal models of hypertension.
SML0025 Safinamide mesylate salt ≥98% (HPLC) Safinamide is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. In addition, safinamide is voltage-dependent sodium and calcium channel blocker. It appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals.
Safinamide mesylate prevents dopamine reuptake and is effective in the treatment of epilepsy and Parkinson′s disease.
T0202 Tocainide hydrochloride ≥98% (HPLC), solid Tocainide hydrochloride is a primary amine analog of lidocaine (lignocaine), used for the treatment of tinnitus. It blocks the sodium channels in the pain-producing foci in the nerve membranes and renders an analgesic effect in trigeminal neuralgia.
Tocainide hydrochloride is a sodium channel blocker; Class IB antiarrhythmic.
T3577 Tolperisone hydrochloride ≥98% (HPLC), solid Tolperisone is an ion channel blocker and centrally acting muscle relaxant.
Tolperisone is derived from piperidine and possesses membrane stabilizing action. It helps in reducing the effect of spasticities associated with the nervous and muscular system. It exhibits muscle relaxant action through attenuating voltage-gated sodium channels in the brain stem.
Tolperisone regulates ionic currents in myelinates axons and subsequently decreases excitability and mediates its antispastic functions3.
T4143 Triamterene ≥99% Weak diuretic with potassium sparing properties; blocks Na+ reuptake in the kidneys.
U6758 UCL 2077 ≥98% (HPLC), solid UCL 2077 is a slow afterhyperpolarization (sAHP) channel blocker.
V5754 Veratridine ≥90% (HPLC), powder Opens voltage-dependent Na+ channels and prevents their inactivation. This, in turn, opens voltage-activated calcium channels, thus increasing intracellular calcium content and inducing neurotransmitter release. Alkaloid neurotoxin which depolarizes excitable tissue; used to increase membrane sodium permeability. Veratridine is cytotoxic to chromaffin cells in vitro.
Veratridine has been used as an insecticide, acting as a paralytic agent with higher toxicity to insects than to mammals.
SML0076 Zoniporide hydrochloride hydrate ≥98% (HPLC) Zoniporide is a potent and selective inhibitor of Na+/H+ exchanger isoform 1 (NHE-1). IC50 = 59 nM at NHE-1, vs. 12,000 nM at NHE-2; Zoniporide inhibits NHE-1-dependent Na+ update with IC50 of 14 nM.
Zoniporide, a selective inhibitor of sodium-hydrogen exchanger isoform 1 (NHE-1) has cardioprotective effects against myocardial injuries and ischemic insults. It inhibits the swelling human platelets and attenuates cardiac contractile dysfunction in rats. Zoniporide might have neurotoxic effects as it causes peripheral sensory axonopathy.